| Identification | Back Directory | [Name]
GSK-LSD1 Dihydrochloride | [CAS]
2102933-95-7 | [Synonyms]
GSK LSD1 dihydrochloride,Monoamine Oxidase,GSK-LSD-1 dihydrochloride,Inhibitor,inhibit,GSK-LSD1,MAO,GSKLSD1 dihydrochloride,Histone Demethylase | [Molecular Formula]
C14H21ClN2 | [MOL File]
2102933-95-7.mol | [Molecular Weight]
252.79 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 1 mg/ml; DMSO: 25 mg/ml; Ethanol: 0.1 mg/ml; PBS (pH 7.2): 10 mg/ml | [form ]
A crystalline solid | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Description]
Lysine-specific demethylase 1 (LSD1) belongs to the family of flavin adenine dinucleotide (FAD)-dependent amine oxidases that include monoamine oxidases (MAOs) and polyamine oxidase (PAO).1 LSD1 specifically demethylates mono- and dimethylated histone H3 lysine 4, resulting in transcriptional repression.2 It also controls the tumor suppressor activity of p53 by demethylating a specific p53 lysine residue (LYS370).3 GSK-LSD1 is an irreversible, mechanism-based inhibitor of LSD1 (IC50 = 16 nM) that is >1,000-fold selective over the closely related FAD-utilizing enzymes LSD2, MAO-A, and MAO-B.4 GSK-LSD1 induces gene expression changes in various cancer cell lines, inhibiting their proliferation (EC50s <5 nM).4 See the Structural Genomics Consortium (SGC) website for more information. | [storage]
Store at -20°C | [References]
1. Shi, Y., Lan, F., Matson, C., et al. Histone demethylation mediated by the nuclear amine oxidase homolog LSD1 Cell 119(7),941-953(2004).
2. Forneris, F., Binda, C., Vanoni, M.A., et al. Human histone demethylase LSD1 reads the histone code J. Biol. Chem. 280(50),41360-41365(2005).
3. Huang, J., Sengupta, R., Espejo, A.B., et al. p53 is regulated by the lysine demethylase LSD1 Nature 449,105-108(2007).
4. Epigenetics probes collection ,(2014). |
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